反应详情

To a 50-mL round-bottomed flask was added 5-(3-(tert-butylamino)-2-methylquinoxalin-5-yl)-1H-pyrazole-3-carboxylic acid (467b) (69 mg, 0.21 mmol), DCM (4 mL), DMF (1 mL), DIPEA (0.15 mL, 0.85 mmol), 2-chloroethanamine hydrochloride (49 mg, 0.42 mmol) (Sigma-Aldrich), and (benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate (110 mg, 0.21 mmol) (Sigma-Aldrich). The reaction mixture was stirred at RT for 16 h and the solvent was completely remover under vacuum. 5-(3-(tert-Butylamino)-2-methylquinoxalin-5-yl)-N-(2-chloroethyl)-1H-pyrazole-3-carboxamide (471a) was taken to next step without purification. m/z (ESI, +ve) 387.0 (M+H)+.

1. custom5-(3-(tert-Butylamino)-2-methylquinoxalin-5-yl)-N-(2-chloroethyl)-1H-pyrazole-3-carboxamide (471a) was taken to next step without purification